1. Field of the Invention
The present invention relates to a high-bioavailability particle coated with fungicide and a polymer, which particularly performs high solubility and bioavailability as the particulate cores are small-sized enough.
2. Related Prior Arts
Itraconazole or (+)-cis-4-[4-[4-[-4[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-1(1-methylpropyl)-3H-1,2,4-triazol-3-one is an oral fungicide which is non-enteric application and locally used as disclosed in U.S. Pat. No. 4,267,179.
However, the compound of U.S. Pat. No. 4,267,179 includes itraconazole which is not water soluble, and thus the bioavailability is unsatisfying. The modified itraconazole compound is easily affected by food and pH value of stomach acid, and therefore effect thereof depends on individuals. The itraconazole performs better solubility at pH<2.0, which does not facilitate solubility in human beings.
To solve the above problem, Taiwan Patent No. 376322 provided “a pellet coated with fungicide and polymer”, which includes: a) a round or spherical core; b) a coating layer including a hydrophilic polymer selected from the group consisting of hydroxypropyl methylcellulose (HPMC), methacrylate, hydroxypropyl cellulose and polyvidone, an a fungicide selected from the group consisting of itraconazole and saperconazole; and c) a closed coating polymer layer of polyethylene glycol. This pellet is characterized in that the core has a diameter ranging from 600 μm to 700 μm (25˜30 mesh); whereby solubility thereof in human beings for treating fungous infection can be promoted.
Unfortunately, though the above pellet coated with fungicide and the polymer can achieve treating effect as expected, aggregation occurs during application because of the too small cores, for example, 30˜35 mesh. The minimum sizes of the cores are therefore limited to 25˜30 mesh, and solubility in human beings is limited, too. As a result, effect of the treatment is still unsatisfying.